Names and pronunciation
rems (brek-san′oh-lone) Zulresso
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Drug reference
rems (brek-san′oh-lone) Zulresso
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Func. class.: Antidepressant
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Chem. class.: GABA modulator
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ACTION: Not fully known but thought to be related to its positive modulation of γ-aminobutyric acid A (GABA-A) recep- tors; GABA is a major inhibitory neu- rotransmitter in the brain
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USES: Postpartum depression
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CONTRAINDICATIONS: Hyper- sensitivity Precautions: Abrupt discontinuation, driving or hazardous activities, breast- feeding, coadministration with other CNS depressants, alcohol use, hypoxia, preg- nancy, renal failure, suicidal ideation
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Black Box Warning: CNS depres- sion, loss of consciousness; requires a specialized setting Black Box Warning: Assess for exces- sive sedation q2hr during planned, non- sleep periods, and stop the infusion if excessive sedation occurs until the symp- tom resolves; thereafter, the infusion may be resumed at the same or lower dose • Available only through the Zulresso Risk Evaluation and Mitigation Strategy (Zulresso REMS) program; risks of seri- ous adverse outcomes (excessive seda- tion or sudden loss/alteration of con- sciousness) Black Box Warning: Requires a special- ized care setting; health care settings must be certified in the REMS program; for further information, including a list of certified health care facilities, visit www. zulressorems.com or call 844-472-4379 • Suicidal ideation: assess for suicidal thoughts and behavior; more common in young adults
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SIDE EFFECTS CNS: Sedation, drowsiness, loss of consciousness, suicidal ideation CV: Tachycardia RESP: Hypoxia INTEG: Injection site reaction
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INTERACTIONS None known
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DOSAGE AND ROUTES Adult females: continuous IV: Give over a total of 60 hr (2.5 days) as follows: 0 to 4 hr: initiate with a dose of 30 mcg/kg/hr; 4 to 24 hr: increase dose to 60 mcg/kg/ hr; 24 to 52 hr: increase dose to 90 mcg/ kg/hr; 52 to 56 hr: decrease dose to 60 mcg/kg/hr; 56 to 60 hr: decrease dose to 30 mcg/kg/hr
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Available forms: Solution for injection 100 mg/20 mL
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Administer: • The vials require dilution • Visually inspect; vial should be clear, colorless without particulate matter and discoloration; do not use discolored vials or vials with particulate matter • 5 infusion bags will be required for the 60-hr infusion; additional bags will be needed for those ≥90 kg • Prepare and store in a polyolefin, non- DEHP, nonlatex bag only; do not use in- line filter • Dilute in the infusion bag immediately after the initial puncture of the vial • Withdraw 20 mL of product from the vial and place in the infusion bag; dilute with 40 mL of sterile water for injection, and further dilute with 40 mL of 0.9% sodium chloride injection (total volume of 100 mL) to achieve a target concentra- tion of 1 mg/mL • Immediately place the infusion bag in refrigerator until use • Give as a continuous IV infusion over a total of 60 hr (2.5 days) via a dedicated line; do not inject other medications into the infusion bag or admix • Use a programmable infusion pump, prime infusion sets with admixture prior to inserting into the pump and connect- ing to the venous catheter • A health care provider must be avail- able on site to continuously monitor • Initiate treatment early enough during B the day to allow for recognition of exces- sive sedation • After the product is diluted, it can be stored in infusion bags under refriger- ated conditions for up to 96 hr • Each diluted product can be used for up to 12 hr of infusion time at room temperature; discard any unused prod- uct after 12 hr of infusion
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Assess: • Monitor for hypoxia using continu- ous pulse oximetry with an alarm; if hypoxia occurs, discontinue and do not reinitiate
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Evaluate: • Therapeutic response: decrease in postpartum depression, improved mood
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • Reason for product and expected result • To discuss all Rx, OTC, herbals and supplements with health care provider • To report pain, inflammation at injec- tion site • Excessive sedation and sudden loss of consciousness: excessive sedation or loss of consciousness can occur; check- ing q2hr for these symptoms will be required; if these occur, tell your health care provider • A family member or caregiver needs to help care for you and your children dur- ing the infusion • Not to drive or engage in hazardous tasks while sleepiness occurs • Not to use alcohol or other CNS de- pressants • Pregnancy/breastfeeding: to identify if pregnancy is planned or suspected or if breastfeeding; if pregnant, register with the National Pregnancy Registry for Anti- depressants at 844-405-6185 or visit https://womensmentalhealth.org/clini- cal-and-research-programs/pregnan- cyregistry/antidepressants/
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PHARMACOKINETICS Extensive distribution into tissues, pro- tein binding >99%, extensively metabo- lized by non-CYP pathways including keto-reduction, glucuronidation, and sulfation; half-life 9 hr; excreted as metabolites in feces (47%) and urine (42%); less than 1% of the drug is excreted as unchanged
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